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HK1167108A1 - Therapeutic agents for reducing parathyroid hormone levels - Google Patents

Therapeutic agents for reducing parathyroid hormone levels

Info

Publication number
HK1167108A1
HK1167108A1 HK12107946.6A HK12107946A HK1167108A1 HK 1167108 A1 HK1167108 A1 HK 1167108A1 HK 12107946 A HK12107946 A HK 12107946A HK 1167108 A1 HK1167108 A1 HK 1167108A1
Authority
HK
Hong Kong
Prior art keywords
sub
compounds
parathyroid hormone
hormone levels
therapeutic agents
Prior art date
Application number
HK12107946.6A
Other languages
Chinese (zh)
Other versions
HK1167108B (en
Inventor
Felix Karim
Amos Baruch
Derek Maclean
Kanad Das
Qun Yin
Original Assignee
Kai Pharmaceuticals, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43527590&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1167108(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Kai Pharmaceuticals, Inc. filed Critical Kai Pharmaceuticals, Inc.
Publication of HK1167108A1 publication Critical patent/HK1167108A1/en
Publication of HK1167108B publication Critical patent/HK1167108B/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/59Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • A61P5/20Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides
    • C07K5/1002Tetrapeptides with the first amino acid being neutral
    • C07K5/1005Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1013Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/08Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X<sub>1</sub> - X<sub>2</sub> - X<sub>3</sub> - X<sub>4</sub> - X<sub>5</sub> - X<sub>6</sub> - X<sub>7</sub>, wherein the X<sub>1</sub> subunit comprises a thiol-containing moiety and the distribution of charge on the X<sub>2</sub>-X<sub>7</sub> subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.
HK12107946.6A 2009-07-29 2010-07-29 Therapeutic agents for reducing parathyroid hormone levels HK1167108B (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US22969509P 2009-07-29 2009-07-29
US61/229,695 2009-07-29
US25581609P 2009-10-28 2009-10-28
US61/255,816 2009-10-28
US31363510P 2010-03-12 2010-03-12
US61/313,635 2010-03-12
PCT/US2010/043792 WO2011014707A2 (en) 2009-07-29 2010-07-29 Therapeutic agents for reducing parathyroid hormone levels

Publications (2)

Publication Number Publication Date
HK1167108A1 true HK1167108A1 (en) 2012-11-23
HK1167108B HK1167108B (en) 2017-12-22

Family

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Also Published As

Publication number Publication date
CA2769525A1 (en) 2011-02-03
JP5270799B2 (en) 2013-08-21
JP2013500990A (en) 2013-01-10
US20240116983A1 (en) 2024-04-11
AU2010278897B2 (en) 2015-02-26
SMT201700014B (en) 2017-03-08
HUE043838T2 (en) 2019-09-30
DK3192520T3 (en) 2019-05-27
US9278995B2 (en) 2016-03-08
SG178143A1 (en) 2012-03-29
CN107674114B (en) 2022-10-25
CA2769525C (en) 2017-02-21
SMT201700014T1 (en) 2017-03-08
US20150175664A1 (en) 2015-06-25
JP2014094967A (en) 2014-05-22
EP2459208A2 (en) 2012-06-06
EP2459208A4 (en) 2014-06-04
CY1121922T1 (en) 2020-10-14
FR17C1009I1 (en) 2017-04-21
SG10201406921SA (en) 2014-11-27
IL217749A (en) 2016-09-29
IL217749A0 (en) 2012-03-29
RU2012107428A (en) 2013-09-10
US9701712B2 (en) 2017-07-11
BR112012002143B8 (en) 2021-05-25
EP3808363B1 (en) 2022-09-07
HRP20190923T1 (en) 2019-10-04
RU2557654C2 (en) 2015-07-27
BR112012002143B1 (en) 2020-12-08
PT2459208T (en) 2017-01-03
US20130150297A1 (en) 2013-06-13
HRP20161614T1 (en) 2017-02-24
JP2013155195A (en) 2013-08-15
LTC2459208I2 (en) 2021-07-12
US8377880B2 (en) 2013-02-19
SI3192520T1 (en) 2019-08-30
US9567370B2 (en) 2017-02-14
US20190194252A1 (en) 2019-06-27
EP4154900B1 (en) 2024-08-28
BR112012002143A2 (en) 2016-11-08
LUC00008I1 (en) 2017-03-16
US8999932B2 (en) 2015-04-07
EP3192520A1 (en) 2017-07-19
CN102711789A (en) 2012-10-03
CY2017010I2 (en) 2017-11-14
HUS1700008I1 (en) 2017-04-28
PT3192520T (en) 2019-06-12
AU2010278897A1 (en) 2012-02-23
EP3192520B1 (en) 2019-03-06
MX2012001213A (en) 2012-06-12
TWI520744B (en) 2016-02-11
EP3808363A1 (en) 2021-04-21
SI2459208T1 (en) 2017-04-26
DK2459208T3 (en) 2017-01-23
TW201116290A (en) 2011-05-16
US20170114095A1 (en) 2017-04-27
RU2557654C3 (en) 2017-07-05
CY2017010I1 (en) 2017-11-14
KR101781841B1 (en) 2017-09-26
KR20120104513A (en) 2012-09-21
LTPA2017007I1 (en) 2017-03-27
NO2017021I1 (en) 2017-05-05
LUC00008I2 (en) 2017-05-30
CN102711789B (en) 2018-06-08
EP3539555A1 (en) 2019-09-18
SMT201900307T1 (en) 2019-07-11
ZA201200726B (en) 2013-05-29
PL3192520T3 (en) 2019-08-30
US20110028394A1 (en) 2011-02-03
US10280198B2 (en) 2019-05-07
ES2607954T3 (en) 2017-04-04
EP3539555B1 (en) 2020-12-30
ES2729051T3 (en) 2019-10-30
US20160159860A1 (en) 2016-06-09
WO2011014707A2 (en) 2011-02-03
US20250163103A1 (en) 2025-05-22
LT2459208T (en) 2017-02-27
US20120178688A1 (en) 2012-07-12
HUE030960T2 (en) 2017-06-28
FR17C1009I2 (en) 2019-04-12
LT3192520T (en) 2019-06-25
EP4154900A1 (en) 2023-03-29
JP5764613B2 (en) 2015-08-19
US20200399309A1 (en) 2020-12-24
PL2459208T3 (en) 2017-05-31
NZ597922A (en) 2015-01-30
CN107674114A (en) 2018-02-09
US20180022777A1 (en) 2018-01-25
WO2011014707A3 (en) 2011-07-07
EP2459208B1 (en) 2016-09-28
CY1118388T1 (en) 2017-06-28

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